CD73

PSB-12379 is a potent Ecto-5'-Nucleotidase (CD73) inhibitor with Kis of 9.03 nM (rat) and 2.21 nM (human).

AB-680 is highly potent, reversible and selective small molecule inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity.

CD73-IN-1 is an inhibitor of CD73 which can be used in the treatment of cancer extracted from patent WO 2017153952 A1, example 80.

MethADP is a specific CD73 inhibitor.

MethADP (sodium salt) is a specific CD73 inhibitor.

LY-3475070 is a potent and selective CD73 Inhibitor with IC50 of 28 nM.

BK50164 is a selective inhibitor of CD73, exhibiting an IC50 of 13.089 μM. It demonstrates a binding affinity to CD99 with a KD of 1.5 μM. This compound exhibits antiproliferative effects and is capable of inducing apoptosis, as well as causing cell cycle arrest in the Sub-G1 phase. BK50164 is valuable in studies focused on tumor immunology and metabolic regulation.

PD-L1/CD-73-IN-1 is a potent inhibitor of PD-L1 and CD73, exhibiting IC50 values of 6 nM and 0.773 μM, respectively. This compound demonstrates significant biological activity by inhibiting tumor cell growth both in vitro and in vivo. It is an essential tool for research applications focused on immune modulation and cancer therapy.

CD73-IN-5 is a potent and selective small molecule inhibitor of CD73, exhibiting an IC50 value of 19 nM. This compound effectively interferes with the enzymatic activity of CD73, which plays a critical role in the production of adenosine in the tumor microenvironment. CD73-IN-5 is utilized in research applications exploring immunomodulation, cancer therapy, and the therapeutic potential of targeting adenosine signaling pathways.

CD73-IN-4 is a selective inhibitor of CD73, functioning through the blockade of adenosine production. With an IC50 of 2.6 nM against human CD73, it demonstrates significant potency in modulating immunosuppressive signals in the tumor microenvironment. This compound is valuable for investigating cancer immunology and exploring therapeutic strategies aimed at enhancing anti-tumor immune responses.

OP-5244 is a potent and orally active inhibitor of CD73, with an IC50 of 0.25 nM. By blocking adenosine production, OP-5244 effectively reverses immunosuppression, making it a valuable tool in cancer research. Its application can aid in the exploration of therapeutic strategies aimed at enhancing anti-tumor immunity.

Dalutrafusp alfa is a bifunctional antibody that targets CD73 and TGF-β, key components involved in the immunosuppressive pathway. This compound modulates immune responses by inhibiting adenosine production and blocking TGF-β signaling. It is primarily utilized in research focused on tumor immunology and the modulation of immune checkpoints. Its unique mechanism allows for exploration in various therapeutic applications, particularly in cancer treatment and autoimmune diseases.

8-BuS-AMP is an inhibitor of NTPDase1, CD73, and CD39, demonstrating an IC50 of 35 μM and a Ki of 0.292 μM for human NTPDase1, alongside Ki values of 1.19 μM for CD73 and 0.847 μM for CD39. This compound interacts with the substrate-binding sites of NTPDase1 and CD73, effectively preventing the conversion of ATP and AMP to adenosine, which promotes the activation and proliferation of human peripheral T lymphocytes. 8-BuS-AMP exhibits robust enzymatic hydrolysis resistance and metabolic stability, and it has no activity against P2Y1 and P2Y12 receptors. This reagent is suitable for investigations into purinergic signaling pathways and cancer research.

ORIC-533 is a selective, orally active inhibitor of CD73 that operates through an AMP-competitive mechanism, demonstrating potent inhibition of adenosine production with a sub-nanomolar affinity (Ka 0.03 nM). This compound has shown significant promise in the context of multiple myeloma, as it enhances the cytotoxic activity of the immune system against tumor cells by reversing immunosuppression, inducing immunogenic cell death, and activating various immune cells including dendritic cells, T cells, and NK cells, while exhibiting minimal toxicity to normal cells. Furthermore, combined administration of ORIC-533 with daratumumab effectively increases intratumoral CD8+ T cell infiltration and substantially inhibits tumor growth in preclinical models.

CD73-IN-11 is a potent inhibitor of CD73, an enzyme responsible for converting extracellular 5'-AMP into adenosine. By inhibiting CD73, this compound disrupts adenosine production, which is known to induce immunosuppressive effects and can promote tumor proliferation and metastasis. CD73-IN-11 is an essential tool for studying tumor-related diseases and investigating the role of adenosine in cancer biology.

CD73-IN-2 is a potent inhibitor of CD73, demonstrating an IC50 value of 0.09 nM. This compound effectively interferes with the enzymatic activity of CD73, which plays a critical role in the regulation of extracellular adenosine levels. CD73-IN-2 is valuable for research applications focused on immuno-oncology, inflammation, and metabolic diseases.

CD73-IN-19 is a potent CD73 inhibitor, exhibiting a 44% inhibition of CD73 enzymatic activity at 100 μM. It effectively counteracts TCR-induced blockade of T cell proliferation at concentrations of 10 μM and 100 μM, highlighting its role in modulating immune responses. Additionally, CD73-IN-19 has been shown to inhibit hA2A receptor activity in HEK-293 cells, with a Ki value of 3.31 μM. This compound demonstrates potential value in studies related to immune disorders and therapeutic interventions.

CD73-IN-10 is a potent inhibitor of CD73, an enzyme that catalyzes the conversion of extracellular 5'-AMP to adenosine. By inhibiting CD73, this compound can reduce the immunosuppressive effects of adenosine, which play a role in tumor proliferation and metastasis. CD73-IN-10 is valuable for research applications focused on tumor biology and the study of tumor-related diseases.

CD73-IN-13 is a potent inhibitor of CD73, an enzyme implicated in tumor growth, angiogenesis, and metastasis. This compound serves as a valuable tool in the investigation of tumor-related diseases, offering insights into the biochemical pathways associated with cancer progression. Researchers can utilize CD73-IN-13 to explore the therapeutic potential of targeting CD73 in various malignancies.

CD73-IN-8 is a potent inhibitor of CD73, an enzyme responsible for converting extracellular 5'-AMP to adenosine. Elevated levels of adenosine are associated with immunosuppression and enhanced tumor growth and metastasis. CD73-IN-8 is valuable for investigating tumor-related diseases and exploring therapeutic strategies aimed at modulating the adenosine pathway in cancer research.

CD73-IN-14 is a potent and selective inhibitor of CD73, exhibiting an IC50 of 0.17 nM. This compound enhances the recruitment of tumor-infiltrating CD8+ T cells and demonstrates significant anti-tumor activity. Additionally, CD73-IN-14 features an alkyne group that enables its use in click chemistry applications, facilitating copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing partners. This reagent is valuable for studies in immuno-oncology and chemical biology, allowing for the exploration of immune modulation and therapeutic strategies.

ZM522 is a potent CD73 inhibitor with an IC50 value of 0.56 μM. This compound enhances immune activity by elevating interferon-γ (INF-γ) levels and modulating T cell activation. ZM522 is suitable for research applications in immunology and cancer therapy, offering potential insights into immune response mechanisms and therapeutic strategies.

MethADP trisodium is a potent inhibitor of CD73, targeting the enzymatic conversion of ATP to adenosine. This compound plays a crucial role in studies investigating the ATP-adenosine signaling pathway and its implications in cancer, immunology, and inflammatory diseases. MethADP trisodium is instrumental for researchers exploring the modulation of adenosine levels and the effects on immune cell function.

MRS4620 is a potent inhibitor of CD73, exhibiting an inhibitory constant (Ki) of 0.436 nM. This compound is primarily utilized in cancer immunology research, where it can help elucidate the role of CD73 in immune regulation and tumor microenvironment modulation. MRS4620 is valuable for studies aimed at enhancing anti-tumor immunity and understanding the mechanisms of immune evasion in cancer.

CD73-IN-9 is a potent inhibitor of CD73, an enzyme that catalyzes the conversion of extracellular 5'-AMP to adenosine. Elevated adenosine levels are associated with immunosuppressive effects and can promote tumor proliferation and metastasis. This compound is valuable for investigating tumor-related diseases and understanding the role of CD73 in cancer biology.

ST80 is an inhibitor of the OTUD4/CD73 interaction. It effectively decreases the protein level of CD73 and enhances its turnover, which reduces the immune evasion capabilities of tumor cells. This results in significant antitumor efficacy, particularly in the context of immunosuppressive triple-negative breast cancer (TNBC), making ST80 valuable for research in cancer immunotherapy.

PSB-0963 is a selective and competitive inhibitor of ecto-5'-nucleotidase (eN or CD73), exhibiting an inhibition constant (Ki) of 150 nM for rat ecto-5'-nucleotidase. This compound demonstrates high selectivity for eN/CD73 over other ectonucleotidases, such as NTPDases 1-3, and P2Y receptors. PSB-0963 is valuable for research involving cancer biology, particularly in studies focused on immune regulation and tumor microenvironment interactions.

CD73-IN-12 is a potent inhibitor of CD73, an enzyme implicated in tumor growth, angiogenesis, and metastasis. This compound serves as a valuable tool for investigating tumor-related diseases and their underlying mechanisms. Additionally, CD73-IN-12 features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it useful for click chemistry applications in biochemical research.

CD73-IN-18 is a potent inhibitor of extracellular 5-nucleotidase (CD73). By blocking CD73 activity, this compound has shown potential in anti-cancer research, enhancing immune responses against tumors. It serves as a valuable tool in studies aimed at understanding tumor microenvironments and developing novel cancer therapies.

CD73-IN-6 is a potent inhibitor of CD73, a key enzyme involved in the adenosine pathway. This compound is essential for investigating the role of CD73 in cancer biology and its potential therapeutic applications. CD73-IN-6 can be utilized in research focused on tumor immunology and the modulation of the tumor microenvironment, providing insights into cancer progression and treatment strategies.

CD73-IN-7 is a potent inhibitor of CD73, an enzyme that catalyzes the conversion of extracellular 5'-AMP to adenosine. Adenosine plays a critical role in immunosuppression and can facilitate tumor proliferation and metastasis. CD73-IN-7 is suitable for research applications focused on tumor biology and the modulation of immune responses in cancer.

MethADP disodium is a specific inhibitor of CD73, an enzyme involved in the regulation of adenosine signaling. By inhibiting CD73 activity, MethADP disodium can impede the production of adenosine, which plays a critical role in immune suppression and tumor progression. This compound is useful for research applications focusing on cancer immunotherapy, inflammation, and metabolic diseases, providing insights into the modulation of the adenosine pathway.

2,4-Dinitrobenzenesulfonic acid is an ecto-5'-nucleotidase (CD73) inhibitor with a Ki value of 63 μM for human enzymes and 144 μM for rat enzymes. This compound effectively inhibits the hydrolysis of adenosine monophosphate (AMP), preventing the production of adenosine. It is primarily utilized in cancer research to study the role of ecto-5'-nucleotidase in tumor biology and therapeutic resistance.